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US 2010/0249109 A1Published application
Substituted tetrahydropyrazolo-pyrido-azepine compounds
AssigneeArQule, Inc.
InventorsJean-Marc Lapierre, Rui-Yang Yang, Nivedita Namdev, Jeffrey S. Link
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Abstract
The present invention relates to substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
Claims21
A compound having formula I:
- or a pharmaceutically acceptable salt or ester thereof, wherein:
- X1, X2 and X3, together with the two carbon atoms numbered “1” and “2”, form a ring selected from
- Rx1 and Rx2 are each independently selected from Qx-Rx;
- Qx is a bond, unsubstituted or substituted C1-C6 alkyl linker, C(O), S(O)2, C(O)NRx′ or S(O)2NRx′;
- and
- Rx and Rx′ are each independently H, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C2-C6 alkenyl, unsubstituted or substituted C6-C10 aryl, unsubstituted or substituted C6-C10 aryl-C1-C6 alkyl, unsubstituted or substituted heteroaryl comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S, unsubstituted or substituted C3-C10 carbocycle or unsubstituted or substituted heterocycle comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S;
- T is CH2 or C(O);
- X is N or C-Q4-R4;
- Y is H, NR6R7, OR6 or SR6, unsubstituted or substituted C1-C6 alkyl, substituted C6-C10 aryl, unsubstituted or substituted heteroaryl comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S, unsubstituted or substituted C3-C10 carbocycle, unsubstituted or substituted heterocycle comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S;
- Q3 and Q4 are each independently a bond, unsubstituted or substituted C1-C6 alkyl linker, C(O), S(O)2, C(O)NR5 or S(O)2NR5;
- R3, R4 and R5 are each independently H, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C2-C6 alkenyl, unsubstituted or substituted C6-C10 aryl, unsubstituted or substituted C6-C10 aryl-C1-C6 alkyl, unsubstituted or substituted heteroaryl comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S, unsubstituted or substituted C3-C10 carbocycle or unsubstituted or substituted heterocycle comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S;
- and
- R6 and R7 are each independently H, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C6-C10 aryl, unsubstituted or substituted heteroaryl comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S, unsubstituted or substituted C3-C10 carbocycle or unsubstituted or substituted heterocycle comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N, O and S.
10 more elements
Dependencies are inferred from the claim text.